Identification of pharmacophore in bioactive metal complexes: Synthesis, spectroscopic characterization and application

Bacteria are amongst the most adaptable organisms on the Earth. The year 2010 was always remarkable for the article published in Lancet Infection Disease by Kumarasamy et al. and the enzyme NDM-1 which makes bacteria resist designed to kill them. Four rhodium(III) chloride complexes with Gatifloxacin have been prepared and characterized by elemental analyses, molar conductance measurements, FTIR, FAB-MS, TGA, 1H NMR and electronic spectral studies. The general formula for complexes are [X]+fac-[RhCl3(L)(GT)]−; where L = H2O, Dimethylsulfoxide (DMSO), Tetramethylenesulfoxide (TMSO); GT = Gatifloxacin and X = Na or [H(DMSO)2]. All complexes are found to possess prominent antibacterial activity against pathogenic Escherichia coli and Mycobacterium tuberculosis in comparison to Gatifloxacin.

Bacteria are amongst the most adaptable organisms on Earth. However, it has poor public image being associated with infectious disease. Metalloantibiotics are promising for amendment of drugs against resist pathogens.Figure optionsDownload as PowerPoint slideHighlights
► Rhodium derivatives with/without sulfoxide ligand were found active against Escherichia coli.
► Sulfoxide-S and Cl remains coordinated in solution state.
► All compounds showed higher potency as compared to Gatifloxacin, DMSO and TMSO.
► Functioning of all compounds is due to the sum of metal ion, GT and pharmacophore.